EP3565549B1 - Inhibiteurs sélectifs d'histone déacétylase pour le traitement d'une maladie humaine - Google Patents

Inhibiteurs sélectifs d'histone déacétylase pour le traitement d'une maladie humaine Download PDF

Info

Publication number
EP3565549B1
EP3565549B1 EP18736068.0A EP18736068A EP3565549B1 EP 3565549 B1 EP3565549 B1 EP 3565549B1 EP 18736068 A EP18736068 A EP 18736068A EP 3565549 B1 EP3565549 B1 EP 3565549B1
Authority
EP
European Patent Office
Prior art keywords
compound
cancer
antibody
aryl
group
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Active
Application number
EP18736068.0A
Other languages
German (de)
English (en)
Other versions
EP3565549A1 (fr
EP3565549A4 (fr
Inventor
Scott Grindrod
Mira Jung
Milton Brown
Anatoly Dritschilo
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Shuttle Pharmaceuticals Inc
Original Assignee
Shuttle Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Shuttle Pharmaceuticals Inc filed Critical Shuttle Pharmaceuticals Inc
Priority to EP22151199.1A priority Critical patent/EP4046989A1/fr
Publication of EP3565549A1 publication Critical patent/EP3565549A1/fr
Publication of EP3565549A4 publication Critical patent/EP3565549A4/fr
Application granted granted Critical
Publication of EP3565549B1 publication Critical patent/EP3565549B1/fr
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Images

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
    • A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
    • A61K31/404—Indoles, e.g. pindolol
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/80—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D211/84—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen directly attached to ring carbon atoms
    • C07D211/86—Oxygen atoms
    • C07D211/88—Oxygen atoms attached in positions 2 and 6, e.g. glutarimide
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca

Claims (15)

  1. Composé ayant la formule (la) ou (Ib) :
    Figure imgb0186
    où R1 est choisi dans le groupe constitué par H et alkyle et aryle facultativement substitués ;
    R2 est choisi dans le groupe constitué par H et alkyle et aryle facultativement substitués ;
    R3 est choisi dans le groupe constitué par H et alkyle et aryle facultativement substitués ;
    X est choisi dans le groupe constitué par -N(R4)C(O)-, -C(O)N(R4)-, -S(O)2N(R4)-, -N(R4)S(O)2-,
    Figure imgb0187
     et
    Figure imgb0188
     , où R4 est choisi dans le groupe constitué par H et alkyle et aryle facultativement substitués ; n est un nombre entier allant de 5 à 7 ;
    ou un sel, solvate, hydrate ou cocristal pharmaceutiquement acceptable de celui-ci.
  2. Composé selon la revendication 1, ayant la formule (II) :
    Figure imgb0189
    où R11 est choisi dans le groupe constitué par H et alkyle et aryle facultativement substitués ;
    R12 est choisi dans le groupe constitué par H et alkyle et aryle facultativement substitués ;
    R13 est choisi dans le groupe constitué par H et alkyle et aryle facultativement substitués ;
    ou un sel, solvate, hydrate ou cocristal pharmaceutiquement acceptable de celui-ci.
  3. Composé selon la revendication 1 ou 2, où le composé est
    Figure imgb0190
     ou un sel, solvate, hydrate ou cocristal pharmaceutiquement acceptable de celui-ci.
  4. Composé selon la revendication 1, ayant la formule (III) :
    Figure imgb0191
    où R21 est choisi dans le groupe constitué par H et alkyle et aryle facultativement substitués ;
    R22 est choisi dans le groupe constitué par H et alkyle et aryle facultativement substitués ;
    R23 est choisi dans le groupe constitué par H et alkyle et aryle facultativement substitués ;
    ou un sel, solvate, hydrate ou cocristal pharmaceutiquement acceptable de celui-ci.
  5. Composé selon la revendication 4, où le composé est
    Figure imgb0192
     ou un sel, solvate, hydrate ou cocristal pharmaceutiquement acceptable de celui-ci.
  6. Utilisation in vitro d'un composé selon l'une quelconque des revendications précédentes comme inhibiteur sélectif de HDAC6.
  7. Composition pharmaceutique comprenant comme agent thérapeutique un composé selon l'une quelconque des revendications 1 à 6 ou un sel, solvate, hydrate ou cocristal pharmaceutiquement acceptable de celui-ci, et un milieu support physiologiquement compatible.
  8. Composition pharmaceutique selon la revendication 7, comprenant un agent thérapeutique supplémentaire qui est un agent chimiothérapeutique ou un agent immunothérapeutique.
  9. Composé selon l'une quelconque des revendications 1 à 5, ou un sel, solvate, hydrate ou cocristal pharmaceutiquement acceptable de celui-ci, pour une utilisation en tant qu'inhibiteur de HDAC dans le traitement d'une maladie soulagée par une inhibition de la protéine histone désacétylase (HDAC) chez un patient.
  10. Composé pour une utilisation selon la revendication 9, où le composé pour une utilisation est le N1-(2,6-dioxopipéridin-3-yl)-N8-hydroxyoctanediamide ou le N1-(2-(2,6-dioxopipéridin-3-yl)-1-oxoisoindolin-4-yl)-N8-hydroxyoctanediamide, ou un sel, solvate, hydrate ou cocristal pharmaceutiquement acceptable de celui-ci.
  11. Composé pour une utilisation selon l'une quelconque des revendications 9 ou 10, où l'inhibiteur de HDAC est un inhibiteur sélectif de HDAC6.
  12. Composé pour une utilisation selon l'une quelconque des revendications 9 à 11, où la maladie est choisie dans le groupe constitué par un cancer, une maladie immunologique, une maladie inflammatoire et une maladie neurologique.
  13. Composé pour une utilisation selon la revendication 12, où le cancer est un cancer HPV positif (+), de préférence un ou plusieurs cancers parmi le cancer du col de l'utérus et le cancer de la tête et du cou.
  14. Composé pour une utilisation selon la revendication 12 ou 13, où la maladie est un cancer et où le traitement comporte en outre l'étape consistant à administrer audit patient une quantité de radiothérapie configurée pour traiter ledit cancer.
  15. Composé pour une utilisation selon l'une quelconque des revendications 9 à 14, où le traitement comprend en outre l'étape consistant à administrer un agent thérapeutique supplémentaire qui est un agent chimiothérapeutique ou un agent immunothérapeutique.
EP18736068.0A 2017-01-09 2018-01-09 Inhibiteurs sélectifs d'histone déacétylase pour le traitement d'une maladie humaine Active EP3565549B1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP22151199.1A EP4046989A1 (fr) 2017-01-09 2018-01-09 Inhibiteurs sélectifs d'histone désacétylase pour le traitement de maladies humaines

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201762444003P 2017-01-09 2017-01-09
PCT/US2018/012971 WO2018129533A1 (fr) 2017-01-09 2018-01-09 Inhibiteurs sélectifs d'histone déacétylase pour le traitement d'une maladie humaine

Related Child Applications (2)

Application Number Title Priority Date Filing Date
EP22151199.1A Division EP4046989A1 (fr) 2017-01-09 2018-01-09 Inhibiteurs sélectifs d'histone désacétylase pour le traitement de maladies humaines
EP22151199.1A Division-Into EP4046989A1 (fr) 2017-01-09 2018-01-09 Inhibiteurs sélectifs d'histone désacétylase pour le traitement de maladies humaines

Publications (3)

Publication Number Publication Date
EP3565549A1 EP3565549A1 (fr) 2019-11-13
EP3565549A4 EP3565549A4 (fr) 2020-09-09
EP3565549B1 true EP3565549B1 (fr) 2022-03-09

Family

ID=62791028

Family Applications (2)

Application Number Title Priority Date Filing Date
EP22151199.1A Pending EP4046989A1 (fr) 2017-01-09 2018-01-09 Inhibiteurs sélectifs d'histone désacétylase pour le traitement de maladies humaines
EP18736068.0A Active EP3565549B1 (fr) 2017-01-09 2018-01-09 Inhibiteurs sélectifs d'histone déacétylase pour le traitement d'une maladie humaine

Family Applications Before (1)

Application Number Title Priority Date Filing Date
EP22151199.1A Pending EP4046989A1 (fr) 2017-01-09 2018-01-09 Inhibiteurs sélectifs d'histone désacétylase pour le traitement de maladies humaines

Country Status (5)

Country Link
US (1) US11034667B2 (fr)
EP (2) EP4046989A1 (fr)
CA (1) CA3049435A1 (fr)
ES (1) ES2914123T3 (fr)
WO (1) WO2018129533A1 (fr)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2914123T3 (es) 2017-01-09 2022-06-07 Shuttle Pharmaceuticals Inc Inhibidores selectivos de la histona desacetilasa para el tratamiento de una enfermedad humana
US11584733B2 (en) 2017-01-09 2023-02-21 Shuttle Pharmaceuticals, Inc. Selective histone deacetylase inhibitors for the treatment of human disease
WO2018165520A1 (fr) 2017-03-10 2018-09-13 Vps-3, Inc. Composés inhibiteurs de métalloenzymes
WO2021092153A1 (fr) * 2019-11-06 2021-05-14 Dana-Farber Cancer Institute, Inc. Agents de dégradation sélectifs d'histone désacétylases 6/8 (hdac6/8) et leurs procédés d'utilisation
IL307883A (en) 2021-04-23 2023-12-01 Tenaya Therapeutics Inc HDAC6 inhibitors for use in the treatment of dilated myocardial disease
EP4333841A1 (fr) 2021-05-04 2024-03-13 Tenaya Therapeutics, Inc. 2-fluoroalkyl-1,3,4-oxadiazol-5-yl-thiazol, inhibiteurs de hdac6 pour utilisation dans le traitement des maladies métaboliques et de l'icfep

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105524043B (zh) * 2016-01-05 2018-08-14 中国药科大学 内酰胺类组蛋白去乙酰化酶抑制剂

Family Cites Families (83)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BE627473A (fr) 1962-01-24
US3968249A (en) 1963-01-22 1976-07-06 E. R. Squibb & Sons, Inc. Method of treating malignant neoplastic disease
JPS6052708B2 (ja) 1976-12-24 1985-11-20 エーザイ株式会社 ５−フルオロウラシル系化合物およびそれを含有する抗腫瘍剤
US4526988A (en) 1983-03-10 1985-07-02 Eli Lilly And Company Difluoro antivirals and intermediate therefor
DE3572982D1 (en) 1984-03-06 1989-10-19 Takeda Chemical Industries Ltd Chemically modified lymphokine and production thereof
IL77133A (en) 1984-12-04 1991-01-31 Lilly Co Eli Antineoplastic pharmaceutical compositions containing pentofuranoside derivatives,some new such compounds and their preparation
US5023252A (en) 1985-12-04 1991-06-11 Conrex Pharmaceutical Corporation Transdermal and trans-membrane delivery of drugs
US5723147A (en) 1987-02-23 1998-03-03 Depotech Corporation Multivesicular liposomes having a biologically active substance encapsulated therein in the presence of a hydrochloride
US5001139A (en) 1987-06-12 1991-03-19 American Cyanamid Company Enchancers for the transdermal flux of nivadipine
US4992445A (en) 1987-06-12 1991-02-12 American Cyanamid Co. Transdermal delivery of pharmaceuticals
CA1327358C (fr) 1987-11-17 1994-03-01 Morio Fujiu Derives fluorocytidine
EP0401384B1 (fr) 1988-12-22 1996-03-13 Kirin-Amgen, Inc. Facteur de stimulation de colonies de granulocytes modifies chimiquement
US5384310A (en) 1989-05-23 1995-01-24 Southern Research Institute 2'-fluoro-2-haloarabinoadinosines and their pharmaceutical compositions
DE3920358A1 (de) 1989-06-22 1991-01-17 Behringwerke Ag Bispezifische und oligospezifische, mono- und oligovalente antikoerperkonstrukte, ihre herstellung und verwendung
KR0162654B1 (ko) 1989-12-11 1998-11-16 알렌 제이. 시니스갤리 N-(피롤로[2,3-d]피리미딘-3-일아크릴)-글루타민산 유도체
ATE297465T1 (de) 1991-11-25 2005-06-15 Enzon Inc Verfahren zur herstellung von multivalenten antigenbindenden proteinen
US5714350A (en) 1992-03-09 1998-02-03 Protein Design Labs, Inc. Increasing antibody affinity by altering glycosylation in the immunoglobulin variable region
TW254946B (fr) 1992-12-18 1995-08-21 Hoffmann La Roche
AU671491B2 (en) 1992-12-18 1996-08-29 F. Hoffmann-La Roche Ag N-oxycarbonyl substituted 5'-deoxy-5-fluorcytidines
US5455044A (en) 1993-05-14 1995-10-03 Depotech Corporation Method for treating neurological disorders
US5476932A (en) 1994-08-26 1995-12-19 Hoffmann-La Roche Inc. Process for producing N4-acyl-5'-deoxy-5-fluorocytidine derivatives
US6083903A (en) 1994-10-28 2000-07-04 Leukosite, Inc. Boronic ester and acid compounds, synthesis and uses
US5635517B1 (en) 1996-07-24 1999-06-29 Celgene Corp Method of reducing TNFalpha levels with amino substituted 2-(2,6-dioxopiperidin-3-YL)-1-oxo-and 1,3-dioxoisoindolines
US6281230B1 (en) 1996-07-24 2001-08-28 Celgene Corporation Isoindolines, method of use, and pharmaceutical compositions
US5939098A (en) 1996-09-19 1999-08-17 Schering Corporation Cancer treatment with temozolomide
US5962521A (en) 1997-04-04 1999-10-05 Guilford Pharmaceuticals Inc. Hydroxamic acid derivatives
US6849616B1 (en) 1998-03-27 2005-02-01 Pharmacia Italia S.P.A. Methods to potentiate intravenous estramustine phosphate
PT1071700E (pt) 1998-04-20 2010-04-23 Glycart Biotechnology Ag Modificação por glicosilação de anticorpos para melhorar a citotoxicidade celular dependente de anticorpos
US6045501A (en) 1998-08-28 2000-04-04 Celgene Corporation Methods for delivering a drug to a patient while preventing the exposure of a foetus or other contraindicated individual to the drug
US6316435B2 (en) 1999-02-24 2001-11-13 Supergen, Inc. Combination therapy for lymphoproliferative diseases
PT1914244E (pt) 1999-04-09 2013-07-26 Kyowa Hakko Kirin Co Ltd Processo para regular a actividade de moléculas funcionais sob o ponto de vista imunológico
US7629360B2 (en) 1999-05-07 2009-12-08 Celgene Corporation Methods for the treatment of cachexia and graft v. host disease
WO2002002093A2 (fr) 2000-06-30 2002-01-10 Eli Lilly And Company Nouvelles polytherapies aux antifolates
DE60138658D1 (de) 2000-09-29 2009-06-18 Topotarget Uk Ltd Carbaminsäurederivate enthaltend eine Amidgruppe zur Behandlung von Malaria
US6315720B1 (en) 2000-10-23 2001-11-13 Celgene Corporation Methods for delivering a drug to a patient while avoiding the occurrence of an adverse side effect known or suspected of being caused by the drug
AU2002243646B2 (en) 2001-01-25 2006-06-22 The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Formulation of boronic acid compounds
PL414997A1 (pl) 2001-02-19 2016-02-29 Novartis Ag Zastosowanie 40-O-(2-hydroksyetylo)-rapamycyny do leczenia guzów litych nerki
EP1443961B1 (fr) 2001-10-25 2009-05-06 Genentech, Inc. Compositions de glycoproteine
JPWO2003085107A1 (ja) 2002-04-09 2005-08-11 協和醗酵工業株式会社 ゲノムが改変された細胞
US7968569B2 (en) 2002-05-17 2011-06-28 Celgene Corporation Methods for treatment of multiple myeloma using 3-(4-amino-1-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione
US8404717B2 (en) 2002-10-15 2013-03-26 Celgene Corporation Methods of treating myelodysplastic syndromes using lenalidomide
US8404716B2 (en) 2002-10-15 2013-03-26 Celgene Corporation Methods of treating myelodysplastic syndromes with a combination therapy using lenalidomide and azacitidine
US7189740B2 (en) 2002-10-15 2007-03-13 Celgene Corporation Methods of using 3-(4-amino-oxo-1,3-dihydro-isoindol-2-yl)-piperidine-2,6-dione for the treatment and management of myelodysplastic syndromes
US20040152632A1 (en) 2002-11-06 2004-08-05 Wyeth Combination therapy for the treatment of acute leukemia and myelodysplastic syndrome
US7842835B2 (en) 2003-07-07 2010-11-30 Georgetown University Histone deacetylase inhibitors and methods of use thereof
UA83504C2 (en) 2003-09-04 2008-07-25 Селджин Корпорейшн Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione
US8188067B2 (en) 2004-04-01 2012-05-29 Teva Pharmaceutical Industries Ltd. Formulations of 6-mercaptopurine
CA2574035A1 (fr) 2004-07-19 2006-02-23 Sandro Belvedere Inhibiteurs de l'histone deacetylase
CA2970873C (fr) 2005-05-09 2022-05-17 E. R. Squibb & Sons, L.L.C. Anticorps monoclonaux humains pour mort programmee 1 (mp-1) et procedes pour traiter le cancer en utilisant des anticorps anti-mp-1 seuls ou associes a d'autres immunotherapies
CN104356236B (zh) 2005-07-01 2020-07-03 E.R.施贵宝&圣斯有限责任公司 抗程序性死亡配体1(pd-l1)的人单克隆抗体
CA2659478A1 (fr) 2006-08-03 2008-02-14 Georgetown University Inhibiteurs hdac selectifs d'une isoforme
CL2007002218A1 (es) 2006-08-03 2008-03-14 Celgene Corp Soc Organizada Ba Uso de 3-(4-amino-1-oxo-1,3-dihidro-isoindol-2-il)-piperidina 2,6-diona para la preparacion de un medicamento util para el tratamiento de linfoma de celula de capa.
US20080051380A1 (en) 2006-08-25 2008-02-28 Auerbach Alan H Methods and compositions for treating cancer
WO2008117935A1 (fr) 2007-03-28 2008-10-02 Industry-Academic Cooperation Foundation, Yonsei University Molécules activatrices des cellules nk, cellules nk et compositions pharmaceutiques contenant celles-ci
EP3222634A1 (fr) 2007-06-18 2017-09-27 Merck Sharp & Dohme B.V. Anticorps dirigés contre le récepteur humain de mort programmée pd-1
WO2009014708A2 (fr) 2007-07-23 2009-01-29 Cell Genesys, Inc. Anticorps pd-1 en combinaison avec une cellule sécrétant de la cytokine et leurs procédés d'utilisation
EP2262837A4 (fr) 2008-03-12 2011-04-06 Merck Sharp & Dohme Protéines de liaison avec pd-1
PE20120341A1 (es) 2008-12-09 2012-04-24 Genentech Inc Anticuerpos anti-pd-l1 y su uso para mejorar la funcion de celulas t
WO2011017448A1 (fr) 2009-08-05 2011-02-10 The Trustees Of The University Of Pennsylvania Utilisation d'inhibiteurs de l'histone désacétylase en vue du traitement de maladies auto-immunes
KR101573109B1 (ko) 2009-11-24 2015-12-01 메디뮨 리미티드 Ｂ７―ｈ１에 대한 표적화된 결합 물질
WO2011106650A2 (fr) 2010-02-27 2011-09-01 University Of Pittsburgh - Of The Commonwealth System Of Higher Education Nouveaux antagonistes de p53-mdm2/p53-mdm4 pour traiter une maladie de prolifération
US8907053B2 (en) 2010-06-25 2014-12-09 Aurigene Discovery Technologies Limited Immunosuppression modulating compounds
US9783578B2 (en) 2010-06-25 2017-10-10 Aurigene Discovery Technologies Limited Immunosuppression modulating compounds
WO2012168944A1 (fr) 2011-06-08 2012-12-13 Aurigene Discovery Technologies Limited Composés thérapeutiques pour une immunomodulation
US9512083B2 (en) * 2011-07-20 2016-12-06 The General Hospital Corporation Histone deacetylase 6 selective inhibitors for the treatment of bone disease
AU2012288413B2 (en) 2011-07-24 2016-10-13 Curetech Ltd. Variants of humanized immunomodulatory monoclonal antibodies
LT2785375T (lt) 2011-11-28 2020-11-10 Merck Patent Gmbh Anti-pd-l1 antikūnai ir jų panaudojimas
EP2822957A1 (fr) 2012-03-07 2015-01-14 Aurigene Discovery Technologies Limited Composés peptidomimétiques utilisés comme immunomodulateurs
CA2868408A1 (fr) 2012-03-29 2013-10-03 Aurigene Discovery Technologies Limited Composes cycliques d'immunomodulation provenant de la boucle bc de pd1 humain
US9724331B2 (en) 2012-12-10 2017-08-08 Centogene Ag Use of maleimide derivatives for preventing and treating leukemia
US9308236B2 (en) 2013-03-15 2016-04-12 Bristol-Myers Squibb Company Macrocyclic inhibitors of the PD-1/PD-L1 and CD80(B7-1)/PD-L1 protein/protein interactions
RU2634694C2 (ru) 2013-04-29 2017-11-03 Чонг Кун Данг Фармасьютикал Корп. Новые соединения для селективных ингибиторов гистондеацетилазы и фармацевтическая композиция, включающая такие соединения
HUP1300432A2 (hu) 2013-07-10 2015-01-28 Tamas Kardos Downhill kerékpár szerkezet javított felfüggesztéssel
SG11201601682RA (en) 2013-09-06 2016-04-28 Aurigene Discovery Tech Ltd 1,2,4-oxadiazole derivatives as immunomodulators
RS57559B1 (sr) 2013-09-06 2018-10-31 Aurigene Discovery Tech Ltd 1,3,4-oksadiazol i 1,3,4-tiadiazol derivativi kao imunomodulatori
WO2015036927A1 (fr) 2013-09-10 2015-03-19 Aurigene Discovery Technologies Limited Dérivés peptidomimétiques d'immunomodulation
AU2013400609B9 (en) 2013-09-13 2020-03-05 Beigene Switzerland Gmbh Anti-PD1 antibodies and their use as therapeutics and diagnostics
WO2015044900A1 (fr) 2013-09-27 2015-04-02 Aurigene Discovery Technologies Limited Composés immunomodulateurs thérapeutiques
WO2015100363A1 (fr) * 2013-12-23 2015-07-02 The Trustees Of Columbia University In The City Of New York Inhibiteurs sélectifs de hdac6
US20170266284A1 (en) * 2014-09-18 2017-09-21 Shuttle Pharmaceuticals, Llc Personalized methods for treating disease by radiosensitization
CN107257800B (zh) 2014-12-23 2020-06-30 达纳-法伯癌症研究所股份有限公司 通过双功能分子诱导靶蛋白降解的方法
US9809539B2 (en) 2015-03-03 2017-11-07 Shuttle Pharmaceuticals, Llc Dual function molecules for histone deacetylase inhibition and ataxia telangiectasia mutated activation and methods of use thereof
ES2914123T3 (es) 2017-01-09 2022-06-07 Shuttle Pharmaceuticals Inc Inhibidores selectivos de la histona desacetilasa para el tratamiento de una enfermedad humana

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105524043B (zh) * 2016-01-05 2018-08-14 中国药科大学 内酰胺类组蛋白去乙酰化酶抑制剂

Also Published As

Publication number Publication date
WO2018129533A1 (fr) 2018-07-12
EP3565549A1 (fr) 2019-11-13
US20200071288A1 (en) 2020-03-05
US11034667B2 (en) 2021-06-15
EP4046989A1 (fr) 2022-08-24
CA3049435A1 (fr) 2018-07-12
EP3565549A4 (fr) 2020-09-09
ES2914123T3 (es) 2022-06-07

Similar Documents

Publication Publication Date Title
EP3565549B1 (fr) Inhibiteurs sélectifs d'histone déacétylase pour le traitement d'une maladie humaine
EP3737376B1 (fr) Inhibiteurs sélectifs d'histone déacétylase pour le traitement de maladies humaines
US11771696B2 (en) Methods of treating chronic lymphocytic leukemia and small lymphocytic leukemia using a BTK inhibitor
US20190022092A1 (en) Therapeutic Combinations of a BTK Inhibitor and a GITR Binding Molecule, a 4-1BB Agonist, or an OX40 Agonist
EP3179992B1 (fr) Combinaisons thérapeutiques associant un inhibiteur de btk, un inhibiteur de pd-1 et/ou un inhibiteur de pd-l1
EP3747472A1 (fr) Combinaisons thérapeutiques d'un inhibiteur cd19 et d'un inhibiteur btk
EP2914343B1 (fr) Association d'un anticorps anti-cd20 et d'un inhibiteur sélectif de la pi3 kinase
US11154554B2 (en) Therapeutic combinations of a MEK inhibitor and a BTK inhibitor
WO2015110923A2 (fr) Méthodes de traitement de la leucémie lymphoïde chronique et du lymphome à petits lymphocytes en utilisant un inhibiteur de btk
WO2016128912A1 (fr) Combinaisons thérapeutiques d'un inhibiteur de btk, d'un inhibiteur de pi3k, d'un inhibiteur de jak-2, d'un inhibiteur de pd-1, et/ou d'un inhibiteur de pd-l1
US11584733B2 (en) Selective histone deacetylase inhibitors for the treatment of human disease
US20130338372A1 (en) Substituted Imidazoline Compounds
CN116234797A (zh) 用于治疗癌症的tead的杂环抑制剂
CA3191842A1 (fr) Inhibiteurs de proteine tyrosine phosphatase et leurs methodes d'utilisation
US20190374543A1 (en) Therapeutic Combinations of an Antifolate and a BTK Inhibitor
TW201609099A (zh) 使用布魯頓（Ｂｒｕｔｏｎ）氏酪胺酸激酶（ＢＴＫ）抑制劑以治療慢性淋巴球性白血病和小淋巴球性白血病之方法
US20230159569A1 (en) Dual hdac6/proteasome inhibitors, and methods of use thereof

Legal Events

Date Code Title Description
STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: THE INTERNATIONAL PUBLICATION HAS BEEN MADE

PUAI Public reference made under article 153(3) epc to a published international application that has entered the european phase

Free format text: ORIGINAL CODE: 0009012

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: REQUEST FOR EXAMINATION WAS MADE

17P Request for examination filed

Effective date: 20190807

AK Designated contracting states

Kind code of ref document: A1

Designated state(s): AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR

AX Request for extension of the european patent

Extension state: BA ME

DAV Request for validation of the european patent (deleted)
DAX Request for extension of the european patent (deleted)
A4 Supplementary search report drawn up and despatched

Effective date: 20200806

RIC1 Information provided on ipc code assigned before grant

Ipc: A61K 31/404 20060101AFI20200731BHEP

Ipc: C07D 209/42 20060101ALI20200731BHEP

REG Reference to a national code

Ref country code: HK

Ref legal event code: DE

Ref document number: 40017061

Country of ref document: HK

GRAP Despatch of communication of intention to grant a patent

Free format text: ORIGINAL CODE: EPIDOSNIGR1

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: GRANT OF PATENT IS INTENDED

INTG Intention to grant announced

Effective date: 20210908

GRAS Grant fee paid

Free format text: ORIGINAL CODE: EPIDOSNIGR3

GRAA (expected) grant

Free format text: ORIGINAL CODE: 0009210

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: THE PATENT HAS BEEN GRANTED

AK Designated contracting states

Kind code of ref document: B1

Designated state(s): AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR

REG Reference to a national code

Ref country code: CH

Ref legal event code: EP

Ref country code: AT

Ref legal event code: REF

Ref document number: 1473557

Country of ref document: AT

Kind code of ref document: T

Effective date: 20220315

REG Reference to a national code

Ref country code: DE

Ref legal event code: R096

Ref document number: 602018031982

Country of ref document: DE

REG Reference to a national code

Ref country code: IE

Ref legal event code: FG4D

REG Reference to a national code

Ref country code: ES

Ref legal event code: FG2A

Ref document number: 2914123

Country of ref document: ES

Kind code of ref document: T3

Effective date: 20220607

REG Reference to a national code

Ref country code: LT

Ref legal event code: MG9D

REG Reference to a national code

Ref country code: NL

Ref legal event code: MP

Effective date: 20220309

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: SE

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220309

Ref country code: RS

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220309

Ref country code: NO

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220609

Ref country code: LT

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220309

Ref country code: HR

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220309

Ref country code: BG

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220609

REG Reference to a national code

Ref country code: AT

Ref legal event code: MK05

Ref document number: 1473557

Country of ref document: AT

Kind code of ref document: T

Effective date: 20220309

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: LV

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220309

Ref country code: GR

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220610

Ref country code: FI

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220309

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: NL

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220309

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: SM

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220309

Ref country code: SK

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220309

Ref country code: RO

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220309

Ref country code: PT

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220711

Ref country code: EE

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220309

Ref country code: CZ

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220309

Ref country code: AT

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220309

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: PL

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220309

Ref country code: IS

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220709

Ref country code: AL

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220309

REG Reference to a national code

Ref country code: DE

Ref legal event code: R097

Ref document number: 602018031982

Country of ref document: DE

PLBE No opposition filed within time limit

Free format text: ORIGINAL CODE: 0009261

STAA Information on the status of an ep patent application or granted ep patent

Free format text: STATUS: NO OPPOSITION FILED WITHIN TIME LIMIT

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: DK

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220309

26N No opposition filed

Effective date: 20221212

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: SI

Free format text: LAPSE BECAUSE OF FAILURE TO SUBMIT A TRANSLATION OF THE DESCRIPTION OR TO PAY THE FEE WITHIN THE PRESCRIBED TIME-LIMIT

Effective date: 20220309

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: FR

Payment date: 20230125

Year of fee payment: 6

Ref country code: ES

Payment date: 20230201

Year of fee payment: 6

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: IT

Payment date: 20230120

Year of fee payment: 6

Ref country code: GB

Payment date: 20230127

Year of fee payment: 6

Ref country code: DE

Payment date: 20230127

Year of fee payment: 6

P01 Opt-out of the competence of the unified patent court (upc) registered

Effective date: 20230504

REG Reference to a national code

Ref country code: CH

Ref legal event code: PL

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: LU

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20230109

REG Reference to a national code

Ref country code: BE

Ref legal event code: MM

Effective date: 20230131

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: LI

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20230131

Ref country code: CH

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20230131

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: BE

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20230131

PG25 Lapsed in a contracting state [announced via postgrant information from national office to epo]

Ref country code: IE

Free format text: LAPSE BECAUSE OF NON-PAYMENT OF DUE FEES

Effective date: 20230109

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: ES

Payment date: 20240201

Year of fee payment: 7

PGFP Annual fee paid to national office [announced via postgrant information from national office to epo]

Ref country code: DE

Payment date: 20240129

Year of fee payment: 7

Ref country code: GB

Payment date: 20240129

Year of fee payment: 7